Use of low molecular weight amino alcohols in ophthalmic compositions

• US 6,319,464 B1
• Filed: 05/14/1999
• Issued: 11/20/2001
• Est. Priority Date: 12/13/1996
• Status: Expired due to Term

• Current Assignee: Alcon Research Limited (Nestle SA)
• Original Assignee: Alcon Manufacturing Limited (Alcon Incorporated)
• Inventors: Asgharian, Bahram
• Primary Examiner(s): Warden, Sr., Robert J.
• Assistant Examiner(s): Soubra, Imad
• Application Number:
  US09/308,456
• Time in Patent Office: 921 Days
• Field of Search: 422/1, 422/5, 422/28, 252/546, 514/839, 514/840, 424/78.04
• US Class Current: 422/28
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/13 Amines A61K31/04 takes precedence
• CPC Class Codes: A61K 31/138 Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377
• CPC Class Codes: A61K 33/22 Boron compounds
• CPC Class Codes: A61K 47/18 Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61L 12/147 Alcohols or derivatives thereof aldehydes A61L12/146
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/04 Artificial tears; Irrigation solutions
• CPC Class Codes: A61P 31/02 Local antiseptics

Abstract

The use of low molecular weight amino alcohols in ophthalmic boric solution is described herein. These compounds have been found to enhance the efficacy of antimicrobial preservatives. Particularly preferred amino alcohols are 2-amino-2-methyl-1-propanol (AMP), 2-dimethylamino-2-methyl-1-propanediol (DMAMP), 2-amino-2-ethylpropanol (AMP), 2-amino-2-methyl-1,3-propanediol (AMPD), and 2-amino-1-butanol (AB). The ophthalmic compositions further optionally comprise a borate/polyol buffer system and an alkylamine.

Claims

1. A method of enhancing the anti-microbial activity of an ophthalmic composition containing a borate compound which comprises adding to the composition an effective amount of a low molecular weight amino alcohol, wherein the amino alcohol has a molecular weight of from 60 to 200 grams/mole.

2. A method according to claim 1, wherein the composition further comprises a borate/polyol buffer system.

3. A method according to claim 1 or 2, wherein the amino alcohol is selected from the group consisting of 2-amino-2-methyl-1-propanol (AMP), 2-dimethylamino-methyl-1-propanediol (DMAMP), 2-amino-2-ethyl-1,3-propanediol (AEPD), 2-amino-2-methyl-1,3-propanediol (AMPD), 2-amino-1-butanol (AB).

4. A method according to claim 3, wherein the composition further comprises an alkylamine.

5. A sterile, multi-dose ophthalmic composition comprising an amount of a low molecular weight amino alcohol effective to enhance the anti-microbial activity of a borate containing composition, wherein the amino alcohol has a molecular weight of from 60 to 200 grams/mole.

6. A composition according to claim 5, wherein the composition is adapted for the treatment of contact lenses.

7. A composition according to claim 6, wherein the composition further comprises a borate/polyol buffer system.

8. A composition according to claim 5, wherein the amino alcohol is selected from the group consisting of 2-amino-2-methyl-1-propanol (AMP), 2-dimethylamino-methyl-1-propanediol (DMAMP), 2-amino-2-ethyl- 1,3-propanediol (AEPD), 2-amino-2-methyl-1,3-propanediol (AMPD), 2-amino-1-butanol (AB).

9. A composition according to claim 5, 6, 7 or 8, further comprising an alkylamine.

10. A composition according to claim 9, wherein the alkylamine is an amidoamine.

11. A composition according to claim 5 or 6, wherein the composition is a multi-purpose solution for treating contact lenses and comprises polyquatemium-1, boric acid, sorbitol, sodium chloride, sodium citrate, a nonionic surfactant, disodium edetate, sodium hydroxide, hydrochloric acid, purified water, 2-amino 2-methyl propanol and MAPDA.

12. A composition according to claim 11, wherein the composition comprises:

about 0.001% w/v of polyquaternium-1;

about 0.6% w/v of boric acid;

about 1.2% w/v of sorbitol;

about 0.65% w/v of sodium citrate;

about 0.1% w/v of sodium chloride;

about 0.05% w/v of a nonionic surfactant

about 0.05% w/v of disodium edetate;

about 0.45% of w/v of AMP-95;

about 0.0005% w/v of MAPDA; and

wherein the composition is adjusted to pH 7.8 with sodium hydroxide and hydrochloric acid.